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Class 514/443 - Polycyclo ring system having the hetero ring as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the five-membered sulfur containing
No. of patents: 925
Last issue date: 05/21/2013


          8            
NumberTitleIssue Date
6492394Sulfonamide hydroxamates
A compound of the Formula (I): ##STR1## wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceu...
12/10/2002
6489356Method for treating pain in humans
The present invention relates to Compound T62, pharmaceutically acceptable salts thereof, and their use in medicine as allosteric adenosine A1 receptor enhancers and uses including treatment of pain, for example, persistent chemical pain, neuro...
12/03/2002
6489355Methods of inhibiting the effects of amyloidogenic proteins
This invention encompasses methods for the inhibition of a physiological disorder associated with amyloidogenic proteins, which method comprises administering to a human in need thereof an effective amount of a compound of Formula I ##STR1## wherein ...
12/03/2002
64893543-alkyl substituted pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: ##STR1## (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine ...
12/03/2002
6489335Treatment of ocular disease
A formulation to treat ocular disease such as dry eye disease, as well as other diseases, is disclosed. Tacrolimus is administered either topically or by injection. For topical administration, an amount of about 1 ng to 10 μg may be formulated in an aque...
12/03/2002
6482859Microbicidal N-sulfonylglycin alkynyloxyphenethyl amide derivatives
The invention relates to novel pesticidally active compounds of the general formula I ##STR1## as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1 -C12 alkyl that is unsu...
11/19/2002
6472406Sulfonamidomethyl phosphonate inhibitors of beta-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ଲ-lactamase inhibitors, which are structurally unrelated to the nat...
10/29/2002
6468971Maintaining kidney function during surgery or trauma
Kappa-opioid agonists prevent the impairment of renal function otherwise caused by the combination of gaseous anesthesia and surgery or severe trauma. Not only do these agents preserve renal function and maintain urine output, they also maintain plasma el...
10/22/2002
6465508Preparation and use of ortho-sulfonamido aryl hydroxamic acids as matrix metalloproteinase inhibitors
Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs....
10/15/2002
6444709Heteroethylene compounds and pharmaceutical and cosmetic compositions containing same
The invention relates to novel heteroethynylenic compounds having the general formula (I): ##STR1## as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, r...
09/03/2002
6440958Acrylic and propionic acid compounds, intermediates, processes, compositions, and methods
This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation ...
08/27/2002
6436993Use of RAR antagonists as modulators of hormone mediated processes
In accordance with the present invention, it has been discovered that retinoic acid receptor (RAR) antagonists are capable of modulating processes mediated by other members of the steroid/thyroid hormone receptor superfamily, including permissive receptor...
08/20/2002
6436958Methods of inhibiting autoimmune diseases
A method of inhibiting auto immune diseases comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R1 and R3 are independently hydrogen, --CH3, ##STR2## or...
08/20/2002
6433005Benzofuran and benzothiophene derivatives as anti-inflammatory agents
This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: ##STR1## wherein A is a --CH2 --, --C(O)--, --O--, --S--, --S(O)--, or --S(O)2 -- and the oth...
08/13/2002
6433004Substituted ଲ,γ-anellated lactones
The present invention relates to novel substituted ଲ,γ-fused lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular ...
08/13/2002
6432983Benzothiophene compounds intermediates processes and methods of use
The instant invention provides compound of formula I ##STR1## wherein: R1 is --H, --OH, --O(C1 -C4 alkyl), --O--CO--(C1 -C6 alkyl), --O--CO--O(C1 -C6 alkyl), --O--CO--Ar in which ...
08/13/2002
6432982Benzothiophenes, and formulations and methods using same
The invention provides novel benzothiophenes of the formula: ##STR1## wherein R1 is --H, --OH, --O(C1 -C4 alkyl), --O--CO(C1 -C6 alkyl), --OSO2 (C4 -C6 alkyl, or --OCOAr wh...
08/13/2002
6423751Upregulation of type III endothelial cell nitric oxide synthase by agents that disrupt actin cytoskeletal organization
A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disr...
07/23/2002
6423717Sulphonamide derivatives, process for their preparation, and their use as medicaments
Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments are disclosed. The present compounds are of formula (I) or a salt thereof: ##STR1## wherein: P isbenzothiophene, benzothiadiazole, quinoline, ...
07/23/2002
6420391Fused thiophone derivatives and drugs containing the same as the active ingredient
The present invention relates to a fused thiophene derivative of the formula (I) (wherein all the symbols are defined as described in the specification) and an inhibitor of producing interleukin-6 and/or interleukin-12 comprising the said derivative as an...
07/16/2002
6420413Heterocycloalkylbenzocyclobutane and heteroarylbenzocyclobutane compounds
A compound selected from those of formula (I): ##STR1## wherein: ##STR2## denotes single bond or double bond, n is integer from 1 to 6 inclusive, R1, and R2 represent a group selected from hydrogen, linear or branched (C1 -C
07/16/2002
64171993-benzyl-benzothiophenes
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are a-substituted with ether, thioether amino, hydrazino, cyano or halo that are useful for the treatment of the various medical...
07/09/2002
6417198Methods of inhibiting CNS problems in post-menopausal women
A method of inhibiting one or more CNS disorders in a post-menopausal woman comprising administering to a female human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R1 and R3 are independe...
07/09/2002
6410586Modulators of protein tyrosine phosphatases (PTPases)
The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B. CD45, SHP-1...
06/25/2002
6410579Use of pramipexole for the treatment of addictive disorders
This patent application describes the treatment addictive disorders, psychoactive substance use disorders, intoxication disorders, inhalation disorders, alcohol addiction, tobacco addiction and or nicotine addiction comprising administering a therapeutica...
06/25/2002
6410574Fungicidal composition and method for using the same
The present invention relates to a fungicidal composition obtained by mixing a 1,2,3-thiadiazole derivative of general formula (I) useful as a plant disease controller with at least one fungicide selected from the compounds having a fungicidal activity ag...
06/25/2002
6407100Fungicidal aromatic oximes
The invention relates to novel compounds of the formula ##STR1## in which R1 is C1-4 alkyl and (Y--X) is CH2, C1-2 alkylthio-CH.dbd. or C1-2 alkyl-ON.dbd. and Z is an aldimino or ketimino group, and t...
06/18/2002
6407102Indole derivatives and their use for the treatment of malignant and other diseases based on pathological cell proliferation
The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: ##STR1## pharmaceuticals containing them and their use for the treatment of malignant and other diseases based on pathological cell proliferatio...
06/18/2002
64036152-Aryl-3-aroylbenzo {b} thiophenes useful for the treatment of estrogen deprivation syndrome
This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I: ##STR1##...
06/11/2002
6403614Benzothiophenes
This invention provides novel benzothiophene compounds of formula I: ##STR1## which are useful for the inhibition of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the bre...
06/11/2002
6395755Benzothiophene pharmaceutical compounds
The present invention provides a compound of formula I ##STR1## wherein R1 is H, OH, halo, OCO(C1 -C6 alkyl), OCO(aryl), OSO2 (C4 -C6 alkyl), OCOO(C1 -C6 alkyl), OCOO(aryl)...
05/28/2002
6395719Methods for increasing levels of acetylcholine
The present invention is directed to increasing levels of acetylcholine by the administration of 2-aryl-3-aroylbenzo[b]thiophenes....
05/28/2002
6391916Enediyne derivatives
Novel C3 -substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3 -substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3 -substituted cyc...
05/21/2002
6391901Thrombin inhibitors
This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the ...
05/21/2002
6391897Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
This invention provides substituted compounds of the general formulae: ##STR1## wherein B and E are C or N; D, G and W are O, S, or N; or salt forms thereof, and methods and pharmaceutical compositions for their use in treating disorders related to insuli...
05/21/2002
6380221Ortho-anthranilamide derivatives as anti-coagulants
This invention is directed to compounds of formula (III): ##STR1## wherein B, C, D, E, R1, R2 and R3 are disclosed herein. These components are disclosed as being useful as anti-coagulants....
04/30/2002
6376534Compounds useful in pain management
Compounds of general formula I ##STR1## are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the ...
04/23/2002
6372779Anti-inflammatory compounds
This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: ##STR1##...
04/16/2002
6362216Compounds which inhibit tryptase activity
The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell ac...
03/26/2002
635301415-ketal postaglandins for the treatment of glaucoma or ocular hypertension
A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I: ##STR1##...
03/05/2002
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